A convenient synthesis of pseudoceratidine and three analogs for biological evaluation.

被引:12
作者
Behrens, C [1 ]
Christoffersen, MW [1 ]
Gram, L [1 ]
Nielsen, PH [1 ]
机构
[1] DANISH INST FISHERIES RES,DEPT SEAFOOD RES,DK-2800 LYNGBY,DENMARK
关键词
D O I
10.1016/S0960-894X(96)00622-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The recently isolated marine natural product pseudoceratidine (1) has been synthesized from 2-trichloroacetylpyrrole. Bromination in the 4- and 5-position followed by nucleophilic displacement of the trichloromethyl group with spermidine gave 1 in 79% yield. The procedure is general and can easily be adopted to the preparation of other derivatives. This was demonstrated by the synthesis of a 5,5'-didebromo derivative (2) and two analogs (3-4). The compounds 1-4 have been tested for antibacterial activity and the results compared to a previous study. Also activity against the marine brine shrimp Artemia salina is reported. (C) 1997, Elsevier Science Ltd.
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收藏
页码:321 / 326
页数:6
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